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Therapeutic agent for keratoconjunctival disorder

a keratoconjunctival disorder and therapeutic agent technology, applied in the field of keratoconjunctival disorder therapeutic agent, can solve the problems of adversely affecting the normal structure of the epithelium, affecting the function of the stroma, and no report of a pharmacological action of these compounds on eye diseases such as keratoconjunctival disorders, and achieve excellent improvement effect on corneal disorder models

Inactive Publication Date: 2007-03-08
SANTEN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0015] The dose can properly be selected depending on the symptoms, age, dosage form and the like. In the case of an eye drop, it may be instilled once to several times a day at a concentration of from 0.0001 to 1% (w / v), preferably from 0.001 to 1% (w / v) . In the case of an oral preparation, it may be administered once or divided into several times at a dose of generally from 0.1 to 5000 mg per day, preferably from 1 to 1000 mg per day. Advantage of the Invention
[0016] As will be described below, when a test for a therapeutic effect on a corneal damage was carried out, both rosiglitazone and pioglitazone hydrochloride of the present invention were found to exert an excellent improving effect on corneal disorder models. Therefore they are useful as a therapeutic agent for a keratoconjunctival disorder such as dry eyes, corneal ulcer, keratitis or conjunctivitis.

Problems solved by technology

Keratoconjunctival disorders caused due to a variety of diseases such as corneal ulcer, keratitis, conjunctivitis, dry eyes and the like may adversely affect normal architecture of epithelium, and furthermore, may impair structures and functions of the stroma and endothelium, when the repair of these disorders is retarded, alternatively when these disorders are prolonged without making repair on some grounds.
However, there has been no report in which a pharmacological action of these compounds on an eye disease such as a keratoconjunctival disorder is studied.

Method used

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  • Therapeutic agent for keratoconjunctival disorder

Examples

Experimental program
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preparation examples

[0032] Hereinafter, representative formulation examples using rosiglitazone or pioglitazone will be shown.

preparation example 1

[0033]

In 100 ml,Rosiglitazoneā€‚10 mgSodium Chloride900 mgSterile purified waterq.s.

[0034] By altering the amount of rosiglitazone to be added, an eye drop at a concentration of 0.001% (w / v), 0.03% (w / v), 0.1% (w / v), 0.3% (w / v), 1.0% (w / v), or 3.0% (w / v) can be prepared.

preparation example 2

[0035]

In 100 ml,Pioglitazone hydrochloride100 mgSodium Chloride800 mgDisodium hydrogen phosphate100 mgSodium dihydrogen phosphateq.s.Sterile purified waterq.s.

[0036] By altering the amount of pioglitazone hydrochloride to be added, an eye drop at a concentration of 0.05% (w / v), 0.3% (w / v), 0.5% (w / v), 1.5% (w / v), or 3% (w / v) can be prepared.

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Abstract

An object of the present invention is to search a new medicinal use of 5-[p-[2-(methyl-2-pyridylamino) ethoxy]benzyl]-2,4-thiazolidinedione and 5-[[4-[2-(5-ethyl-2-pyridinyl)ethoxy]phenyl]methyl]-2,4-thiazolidinedione. 5-[p-[2-(methyl-2-pyridylamino)ethoxy]benzyl]-2,4-thiazolidinedione, 5-[[4-[2-(5-ethyl-2-pyridinyl)ethoxy]phenyl]methyl]-2,4-thiazolidinedione or a salt thereof exerts an excellent improving effect on corneal disorder models, therefore, it is useful as a therapeutic agent for a keratoconjunctival disorder such as dry eyes, corneal ulcer, keratitis or conjunctivitis.

Description

[0001] This application is a continuation-in-part application of International Application PCT / JP2005 / 008584 (not published in English) filed May 11, 2005.TECHNICAL FIELD [0002] The present invention relates to a therapeutic agent for a keratoconjunctival disorder such as dry eyes, corneal ulcer, keratitis or conjunctivitis, comprising as an active ingredient, 5-[p-[2-(methyl-2-pyridylamino)ethoxy]benzyl]-2,4-thiazolidinedione, 5-[[4-[2-(5-ethyl-2-pyridinyl)ethoxy]phenyl]methyl]-2,4-thiazolidinedione, both of which are a thiazolidinedione derivative, or a salt thereof. BACKGROUND ART [0003] Cornea is a transparent avascular tissue having a diameter of about 1 cm and a thickness of about 1 mm, while conjunctiva is a mucosal membrane covering the eyeball surface posterior to the corneal margin, and the back face of the eyelid. The cornea and the conjunctiva are known to significantly affect the visual function. Keratoconjunctival disorders caused due to a variety of diseases such as c...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/4439A61K9/00A61K9/06A61K9/08A61P27/02A61P27/04A61P27/14C07D417/12
CPCA61K31/4439A61K9/0048A61P27/02A61P27/04A61P27/14C07D417/12
Inventor NAKAMURA, MASATSUGUHIRAI, SHIN-ICHIRO
Owner SANTEN PHARMA CO LTD
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